Determination of a novel B-Raf(V600E) and EGFR dual inhibitor in rat plasma by HPLC-MS/MS and its application in a pharmacokinetic study.

Abstract The EGFR and B-Raf V600E dual inhibition is a promising strategy in treatment of colorectal cancer patients with B-Raf V600E mutation. Previously, compound 3 was designed and synthesized as a novel B-Raf V600E and EGFR dual inhibitor with highly potency in both kinase and cell based assay. Herein, a sensitive and rapid HPLC–MS/MS quantitative method was developed and validated for the further pharmacokinetic evaluation of compound 3 in rats.